HRP20220215T1 - Inhibitori mcl-1 - Google Patents
Inhibitori mcl-1 Download PDFInfo
- Publication number
- HRP20220215T1 HRP20220215T1 HRP20220215TT HRP20220215T HRP20220215T1 HR P20220215 T1 HRP20220215 T1 HR P20220215T1 HR P20220215T T HRP20220215T T HR P20220215TT HR P20220215 T HRP20220215 T HR P20220215T HR P20220215 T1 HRP20220215 T1 HR P20220215T1
- Authority
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- Croatia
- Prior art keywords
- image
- alkyl
- heteroalkyl
- cycloalkyl
- membered heterocyclyl
- Prior art date
Links
- 101001056180 Homo sapiens Induced myeloid leukemia cell differentiation protein Mcl-1 Proteins 0.000 title 1
- 102100026539 Induced myeloid leukemia cell differentiation protein Mcl-1 Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 27
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 25
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 23
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 13
- 150000002431 hydrogen Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 229910003827 NRaRb Inorganic materials 0.000 claims 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- -1 -(CH2CH2O)pR7 Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D267/16—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D267/20—[b, f]-condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C381/00—Compounds containing carbon and sulfur and having functional groups not covered by groups C07C301/00 - C07C337/00
- C07C381/10—Compounds containing sulfur atoms doubly-bound to nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Hematology (AREA)
- Oncology (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862671306P | 2018-05-14 | 2018-05-14 | |
| US201862749918P | 2018-10-24 | 2018-10-24 | |
| PCT/US2019/032053 WO2019222112A1 (en) | 2018-05-14 | 2019-05-13 | Mcl-1 inhibitors |
| EP19728793.1A EP3793565B1 (en) | 2018-05-14 | 2019-05-13 | Mcl-1 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20220215T1 true HRP20220215T1 (hr) | 2022-04-29 |
Family
ID=66770559
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20220215TT HRP20220215T1 (hr) | 2018-05-14 | 2019-05-13 | Inhibitori mcl-1 |
Country Status (30)
| Country | Link |
|---|---|
| US (5) | US10703733B2 (enExample) |
| EP (2) | EP4029868A1 (enExample) |
| JP (3) | JP6899975B2 (enExample) |
| KR (4) | KR102732008B1 (enExample) |
| CN (2) | CN112118845B (enExample) |
| AU (3) | AU2019269391B2 (enExample) |
| BR (1) | BR112020021648A2 (enExample) |
| CA (1) | CA3099152C (enExample) |
| CL (1) | CL2020002919A1 (enExample) |
| CO (1) | CO2020014009A2 (enExample) |
| CR (1) | CR20200544A (enExample) |
| CY (1) | CY1125065T1 (enExample) |
| DK (1) | DK3793565T3 (enExample) |
| ES (1) | ES2907923T3 (enExample) |
| HR (1) | HRP20220215T1 (enExample) |
| HU (1) | HUE057852T2 (enExample) |
| IL (2) | IL291430B2 (enExample) |
| LT (1) | LT3793565T (enExample) |
| MX (1) | MX2020012137A (enExample) |
| MY (1) | MY198871A (enExample) |
| PE (1) | PE20210004A1 (enExample) |
| PH (1) | PH12020551881A1 (enExample) |
| PL (1) | PL3793565T3 (enExample) |
| PT (1) | PT3793565T (enExample) |
| SG (1) | SG11202010964VA (enExample) |
| SI (1) | SI3793565T1 (enExample) |
| TW (4) | TWI813957B (enExample) |
| UA (1) | UA125163C2 (enExample) |
| WO (1) | WO2019222112A1 (enExample) |
| ZA (1) | ZA202007007B (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102732008B1 (ko) | 2018-05-14 | 2024-11-20 | 길리애드 사이언시즈, 인코포레이티드 | Mcl-1 억제제 |
| EP3643711A1 (en) | 2018-10-24 | 2020-04-29 | Bayer Animal Health GmbH | New anthelmintic compounds |
| ES2987630T3 (es) | 2019-07-09 | 2024-11-15 | Janssen Pharmaceutica Nv | Derivados de espirociclos macrocíclicos como inhibidores de MCL-1 |
| US11795223B2 (en) | 2019-10-18 | 2023-10-24 | Forty Seven, Inc. | Combination therapies for treating myelodysplastic syndromes and acute myeloid leukemia |
| MX2022005123A (es) | 2019-10-31 | 2022-05-30 | Forty Seven Inc | Tratamiento basado en anti-cd47 y anti-cd20 para cancer hematologico. |
| TWI778443B (zh) | 2019-11-12 | 2022-09-21 | 美商基利科學股份有限公司 | Mcl1抑制劑 |
| US11325891B2 (en) | 2019-11-26 | 2022-05-10 | Gilead Sciences, Inc. | Processes and intermediates for preparing MCL1 inhibitors |
| MX2022007930A (es) | 2019-12-24 | 2022-08-08 | Carna Biosciences Inc | Compuestos moduladores de diacilglicerol quinasa. |
| US20230212191A1 (en) * | 2020-04-16 | 2023-07-06 | Prelude Therapeutics, Incorporated | Spiro-sulfonimidamide derivatives as inhibitors of myeloid cell leukemia-1 (mcl-1) protein |
| US20230219906A1 (en) | 2020-06-10 | 2023-07-13 | Janssen Pharmaceutica Nv | Macrocyclic-2-amino-3-fluoro-but-3-enamides as inhibitors of mcl-1 |
| CN116457334A (zh) * | 2020-11-19 | 2023-07-18 | 吉利德科学公司 | 用于制备大环mcl1抑制剂的方法和中间体 |
| ES3026771T3 (en) | 2020-12-17 | 2025-06-12 | Janssen Pharmaceutica Nv | Macrocyclic branched 3-fluoro-but-3-enamides as inhibitors of mcl-1 |
| TW202302145A (zh) | 2021-04-14 | 2023-01-16 | 美商基利科學股份有限公司 | ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症 |
| AU2022267722A1 (en) | 2021-04-26 | 2023-12-14 | Janssen Pharmaceutica Nv | Macrocyclic 2-allyltetrahydrofurans as inhibitors of mcl-1 |
| US20220389394A1 (en) | 2021-05-18 | 2022-12-08 | Gilead Sciences, Inc. | METHODS OF USING FLT3L-Fc FUSION PROTEINS |
| WO2022261310A1 (en) | 2021-06-11 | 2022-12-15 | Gilead Sciences, Inc. | Combination mcl-1 inhibitors with anti-body drug conjugates |
| CN117651554A (zh) * | 2021-06-11 | 2024-03-05 | 吉利德科学公司 | Mcl-1抑制剂与抗癌剂的组合 |
| WO2022271684A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| JP7686086B2 (ja) | 2021-06-23 | 2025-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | ジアシルグリエルコール（ｄｉａｃｙｌｇｌｙｅｒｃｏｌ）キナーゼ調節化合物 |
| WO2022271659A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| MX2024005928A (es) | 2021-11-16 | 2024-06-04 | Janssen Pharmaceutica Nv | 2-amino-but-3-enamidas macrociclicas como inhibidores de mcl-1. |
| JP2025509662A (ja) | 2022-03-24 | 2025-04-11 | ギリアード サイエンシーズ， インコーポレイテッド | Ｔｒｏｐ－２発現がんを治療するための併用療法 |
| TWI876305B (zh) | 2022-04-05 | 2025-03-11 | 美商基利科學股份有限公司 | 用於治療結腸直腸癌之組合療法 |
| US12162896B2 (en) * | 2022-05-04 | 2024-12-10 | Gilead Sciences, Inc. | Salts and polymorphs of certain MCL-1 inhibitors |
| WO2024064668A1 (en) | 2022-09-21 | 2024-03-28 | Gilead Sciences, Inc. | FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY |
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